产品说明书

Phenacetin

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Chemical Structure| 62-44-2 同义名 : N-(4-乙氧基苯基)乙酰胺 ;Acetophenetidin;p-Acetophenetidide;NSC 7651;4′-Ethoxyacetanilide
CAS号 : 62-44-2
货号 : A159869
分子式 : C10H13NO2
纯度 : 98%
分子量 : 179.22
MDL号 : MFCD00009094
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(585.89 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
靶点
  • COX

描述 Phenacetin is a non-opioid analgesic without anti-inflammatory properties, inhibits COX-3 activity[3]. Phenacetin has been linked to renal papillary necrosis in human beings[4]. Since a major portion of a dose of phenacetin is rapidly metabolised to paracetamol, it seems possible that phenacetin owes some of its therapeutic activity to its main metabolite, paracetamol, whereas its most troublesome side effect (methaemoglobinaemia) is due to another metabolite, p-phenetidine[5]. Phenacetin treatment caused considerable nephrotoxicity and hepatotoxicity. Bioisosteric replacement of amide bond by 1,2,3-triazole in the phenacetin moiety yields conjugates with superior efficacy and diminished toxicity[6]. Combination analgesics containing phenacetin increase the risk of development of tumours in the renal pelvis. Phenacetin also increases the risk of development of cancer of the bladder[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.58mL

1.12mL

0.56mL

27.90mL

5.58mL

2.79mL

55.80mL

11.16mL

5.58mL

参考文献

[1]Brix AE. Renal papillary necrosis. Toxicol Pathol. 2002 Nov-Dec;30(6):672-4.

[2]TAN GH, RABBINO MD, et al. IS PHENACETIN A NEPHROTOXIN?A REPORT ON TWENTY-THREE USERS OF THE DRUG. Calif Med. 1964 Aug;101:73-7.

[3]Chandrasekharan NV, Dai H, Roos KL, et al. COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs: cloning, structure, and expression. Proc Natl Acad Sci U S A. 2002;99(21):13926-13931

[4]Brix AE. Renal papillary necrosis. Toxicol Pathol. 2002;30(6):672-674

[5]Clissold SP. Paracetamol and phenacetin. Drugs. 1986;32 Suppl 4:46-59

[6]Sahu A, Das D, Agrawal RK, Gajbhiye A. Bio-isosteric replacement of amide group with 1,2,3-triazole in phenacetin improves the toxicology and efficacy of phenacetin-triazole conjugates (PhTCs). Life Sci. 2019;228:176-188

[7]Nørgaard N, Jensen OM. Fenacetin, paracetamol og blaerecancer [Phenacetin, paracetamol and bladder cancer]. Ugeskr Laeger. 1990;152(49):3687-3691